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公开(公告)号：US20120258949A1
公开(公告)日：2012-10-11
申请号：US13446861
申请日：2012-04-13
申请人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
发明人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
IPC分类号： A61K31/407 , A61K31/438 , A61K31/55 , A61K31/397 , C07D498/10 , A61K31/537 , A61P35/00 , A61P25/00 , A61P29/00 , A61P31/00 , A61P11/00 , A61P37/00 , A61P9/00 , A61P21/00 , A61P17/06 , C07D491/107
CPC分类号： A61K31/397 , A61K31/407 , A61K31/438 , A61K31/537 , A61K31/55 , C07D491/107 , C07D498/10
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C═R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：m和n独立地为0或1至4的整数; p为0或1至3的整数，条件是当p为零时，n和m不能同时为1; R是氢; 任选被C 3 -C 8环烷基，C 6 -C 10芳基或杂（C 2 -C 9）芳基取代的C 1 -C 6烷基; （CO）R2; （SO2）R3; C3-C8环烷基; C6-C10芳基; 或杂（C 2 -C 9）芳基; R1是卤素，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基，C1-C6卤代烷氧基; Y是CH 2或NR 4; Z为C = R5; R2，R3，R4和R5如说明书中进一步定义; 及其药学上可接受的盐。
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公开(公告)号：US08980877B2
公开(公告)日：2015-03-17
申请号：US13446861
申请日：2012-04-13
申请人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
发明人： Mario Varasi , Florian Thaler , Raffaella Amici , Agnese Abate , Maria Carmela Fulco , Saverio Minucci , Ciro Mercurio
IPC分类号： A61K31/407 , A61K31/438 , A61K31/55 , C07D491/107 , A61K31/397 , A61K31/537 , C07D498/10
CPC分类号： A61K31/397 , A61K31/407 , A61K31/438 , A61K31/537 , A61K31/55 , C07D491/107 , C07D498/10
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C═R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：m和n独立地为0或1至4的整数; p为0或1至3的整数，条件是当p为零时，n和m不能同时为1; R是氢; 任选被C 3 -C 8环烷基，C 6 -C 10芳基或杂（C 2 -C 9）芳基取代的C 1 -C 6烷基; （CO）R2; （SO2）R3; C3-C8环烷基; C6-C10芳基; 或杂（C 2 -C 9）芳基; R1是卤素，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基，C1-C6卤代烷氧基; Y是CH 2或NR 4; Z为C = R5; R2，R3，R4和R5如说明书中进一步定义; 及其药学上可接受的盐。
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公开(公告)号：US08592444B2
公开(公告)日：2013-11-26
申请号：US12988197
申请日：2009-04-14
申请人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
发明人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
IPC分类号： C07D401/04 , A61K31/438
CPC分类号： C07D498/10 , A61K31/438 , C07D471/10 , C07D491/107 , Y02A50/409 , Y02A50/411
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基，芳基或杂芳基取代的C 1 -C 6烷基; （CO）R3; （SO2）R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或（CO）R5; X是CH 2，氧或NR 6; Y是一个键，CHR7或NR8; Z是氧，CR9R10或C = R11; R3，R4，R5，R6，R7，R8，R9，R10和R11在说明书中进一步定义; 及其药学上可接受的盐。
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公开(公告)号：US20110039840A1
公开(公告)日：2011-02-17
申请号：US12988197
申请日：2009-04-14
申请人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
发明人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
IPC分类号： A61K31/537 , C07D491/10 , A61K31/438 , A61P35/00 , A61P31/18 , A61P25/08 , A61P9/10 , A61P37/00 , A61P17/06 , A61P35/04 , A61P25/16 , A61P25/28 , A61P25/18 , A61P33/06 , A61P33/02 , A61P31/10 , A61P31/12 , C07D498/10 , C07D471/10 , A61K31/527 , A61K31/506
CPC分类号： C07D498/10 , A61K31/438 , C07D471/10 , C07D491/107 , Y02A50/409 , Y02A50/411
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基，芳基或杂芳基取代的C 1 -C 6烷基; （CO）R3; （SO2）R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或（CO）R5; X是CH 2，氧或NR 6; Y是一个键，CHR7或NR8; Z是氧，CR9R10或C = R11; R3，R4，R5，R6，R7，R8，R9，R10和R11在说明书中进一步定义; 及其药学上可接受的盐。
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公开(公告)号：US20140080823A1
公开(公告)日：2014-03-20
申请号：US14088061
申请日：2013-11-22
申请人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
发明人： Mario Varasi , Florian Thaler , Agnese Abate , Giacomo Carenzi , Ciro Mercurio , Saverio Minucci
IPC分类号： C07D498/10 , C07D471/10 , C07D491/107
CPC分类号： C07D498/10 , A61K31/438 , C07D471/10 , C07D491/107 , Y02A50/409 , Y02A50/411
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基，芳基或杂芳基取代的C 1 -C 6烷基; （CO）R3; （SO2）R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或（CO）R5; X是CH 2，氧或NR 6; Y是一个键，CHR7或NR8; Z是氧，CR9R10或C = R11; R3，R4，R5，R6，R7，R8，R9，R10和R11在说明书中进一步定义; 及其药学上可接受的盐。
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